Yang Ji-Ung, Kim Soyeon, Ahn Jae Hun, Kim Min Hwan, Kil Hee Seup, Chi Dae Yoon, Lee Kyo Chul, Lee Yong Jin, Park Ji-Ae
Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea; Department of Medical & Biological Engineering, Kyungpook National University, Daegu, 41566, South Korea.
Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS), Seoul, 01812, South Korea.
Biochem Biophys Res Commun. 2022 Jun 4;607:152-157. doi: 10.1016/j.bbrc.2022.03.136. Epub 2022 Mar 28.
The aim of this work was to evaluate Gd-FC705, a prostate-specific membrane antigen (PSMA)-targeted MRI contrast agent. The r and r relaxivities of Gd-FC705 are 5.94 mMs and 17.77 mMs, respectively, in HSA solution (0.67 mM) at 3 T, which are higher than those of Gd-DOTA. Specific targeting efficacy was found with a 3-fold enhancement between PSMA-negative (PSMA-) and PSMA-positive (PSMA+) cells. The in vivo targeting and bio-distribution of Gd-FC705 were further confirmed using nude mice bearing PC3 human prostate cancer xenografts, which showed a 2-fold increase in the contrast-to-noise ratio (CNR) for PSMA+ tumors compared to PSMA- tumors 1 h post injection and a longer circulation time than Gd-DOTA. These results demonstrate that Gd-FC705 has great potential as a diagnostic agent for prostate cancer.
这项工作的目的是评估钆- FC705，一种靶向前列腺特异性膜抗原（PSMA）的磁共振成像（MRI）造影剂。在3T的人血清白蛋白（HSA）溶液（0.67 mM）中，钆- FC705的纵向弛豫率（r1）和横向弛豫率（r2）分别为5.94 mM⁻¹s⁻¹和17.77 mM⁻¹s⁻¹，高于钆-多胺羧基配合物（Gd-DOTA）。在PSMA阴性（PSMA-）和PSMA阳性（PSMA+）细胞之间发现了3倍的增强，具有特异性靶向效果。使用携带PC3人前列腺癌异种移植瘤的裸鼠进一步证实了钆- FC705的体内靶向性和生物分布，结果显示，注射后1小时，PSMA+肿瘤的对比噪声比（CNR）比PSMA-肿瘤增加了2倍，且循环时间比Gd-DOTA更长。这些结果表明，钆- FC705作为一种前列腺癌诊断剂具有巨大潜力。
